蛋白质-蛋白质相互作用在多种细胞功能中具有重要的作用。靶向蛋白质-蛋白质相互作用已经成为新药发现的重要策略,但发现能阻断蛋白质-蛋白质相互作用的小分子药物是一个巨大的挑战。尽管如此,近年来人们还是发现了许多能调控蛋白质-蛋白质相互作用的小分子。该文主要总结了在病毒进入、细胞凋亡通路和神经退行性疾病等方面的蛋白质-蛋白质相互作用小分子抑制剂的研究进展。 Protein-protein interactions play an important role in a variety of cellular functions. Targeting protein-protein interactions has become an important strategy for new drug discovery, but the discovery of small molecule drugs that block protein-protein interactions is a huge challenge. However, in recent years, many people still found a small number of molecules that can regulate protein-protein interactions. This article summarizes the advances in small molecule inhibitors of protein-protein interactions in terms of viral entry, apoptotic pathways, and neurodegenerative diseases.